RU2670272C2 - Пероральная фармацевтическая композиция, подходящая для повышения эффективности лечения двигательных нарушений - Google Patents
Пероральная фармацевтическая композиция, подходящая для повышения эффективности лечения двигательных нарушений Download PDFInfo
- Publication number
- RU2670272C2 RU2670272C2 RU2014145944A RU2014145944A RU2670272C2 RU 2670272 C2 RU2670272 C2 RU 2670272C2 RU 2014145944 A RU2014145944 A RU 2014145944A RU 2014145944 A RU2014145944 A RU 2014145944A RU 2670272 C2 RU2670272 C2 RU 2670272C2
- Authority
- RU
- Russia
- Prior art keywords
- pharmaceutical composition
- agonist
- composition according
- component
- hpmc
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 31
- 208000019430 Motor disease Diseases 0.000 title claims description 20
- 239000008203 oral pharmaceutical composition Substances 0.000 title description 2
- 229960001360 zolmitriptan Drugs 0.000 claims abstract description 159
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 135
- QWCRAEMEVRGPNT-UHFFFAOYSA-N buspirone Chemical compound C1C(=O)N(CCCCN2CCN(CC2)C=2N=CC=CN=2)C(=O)CC21CCCC2 QWCRAEMEVRGPNT-UHFFFAOYSA-N 0.000 claims abstract description 132
- 229960002495 buspirone Drugs 0.000 claims abstract description 129
- 239000011159 matrix material Substances 0.000 claims abstract description 95
- 239000000556 agonist Substances 0.000 claims abstract description 90
- 102100027499 5-hydroxytryptamine receptor 1B Human genes 0.000 claims abstract description 75
- 102100027493 5-hydroxytryptamine receptor 1D Human genes 0.000 claims abstract description 64
- 102100022738 5-hydroxytryptamine receptor 1A Human genes 0.000 claims abstract description 52
- 239000004480 active ingredient Substances 0.000 claims abstract description 51
- 239000003814 drug Substances 0.000 claims abstract description 51
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims abstract description 51
- 101710138638 5-hydroxytryptamine receptor 1A Proteins 0.000 claims abstract description 50
- 229940044601 receptor agonist Drugs 0.000 claims abstract description 49
- 239000000018 receptor agonist Substances 0.000 claims abstract description 49
- 239000008186 active pharmaceutical agent Substances 0.000 claims abstract description 38
- 239000000126 substance Substances 0.000 claims abstract description 34
- 238000013268 sustained release Methods 0.000 claims abstract description 29
- 239000012730 sustained-release form Substances 0.000 claims abstract description 29
- 230000006735 deficit Effects 0.000 claims abstract description 21
- 101150050738 HTR1B gene Proteins 0.000 claims abstract description 14
- 101150039275 Htr1f gene Proteins 0.000 claims abstract description 11
- 101100321769 Takifugu rubripes htr1d gene Proteins 0.000 claims abstract description 11
- 150000003839 salts Chemical class 0.000 claims abstract description 9
- UTAZCRNOSWWEFR-ZDUSSCGKSA-N zolmitriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1C[C@H]1COC(=O)N1 UTAZCRNOSWWEFR-ZDUSSCGKSA-N 0.000 claims abstract 2
- 239000003826 tablet Substances 0.000 claims description 119
- 208000012661 Dyskinesia Diseases 0.000 claims description 96
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 91
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 91
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 88
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 88
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 87
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 81
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 79
- 101710138639 5-hydroxytryptamine receptor 1B Proteins 0.000 claims description 63
- 101710138068 5-hydroxytryptamine receptor 1D Proteins 0.000 claims description 63
- 239000000203 mixture Substances 0.000 claims description 63
- 102100036311 5-hydroxytryptamine receptor 1F Human genes 0.000 claims description 48
- 101710138086 5-hydroxytryptamine receptor 1F Proteins 0.000 claims description 48
- 229940079593 drug Drugs 0.000 claims description 47
- 238000000576 coating method Methods 0.000 claims description 45
- 239000011248 coating agent Substances 0.000 claims description 40
- 229960003638 dopamine Drugs 0.000 claims description 40
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 39
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 39
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 39
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 39
- 239000008187 granular material Substances 0.000 claims description 34
- 229910052623 talc Inorganic materials 0.000 claims description 32
- 239000000454 talc Substances 0.000 claims description 31
- 239000003723 serotonin 1A agonist Substances 0.000 claims description 29
- 208000018737 Parkinson disease Diseases 0.000 claims description 28
- 102000005962 receptors Human genes 0.000 claims description 27
- 108020003175 receptors Proteins 0.000 claims description 27
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 25
- BNQDCRGUHNALGH-UHFFFAOYSA-N benserazide Chemical compound OCC(N)C(=O)NNCC1=CC=C(O)C(O)=C1O BNQDCRGUHNALGH-UHFFFAOYSA-N 0.000 claims description 18
- 229960000911 benserazide Drugs 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 239000010410 layer Substances 0.000 claims description 16
- 230000037396 body weight Effects 0.000 claims description 14
- 208000016285 Movement disease Diseases 0.000 claims description 12
- 239000002671 adjuvant Substances 0.000 claims description 11
- 108010053303 serotonin 1F receptor Proteins 0.000 claims description 10
- 239000007909 solid dosage form Substances 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 9
- 230000001575 pathological effect Effects 0.000 claims description 9
- 239000000651 prodrug Substances 0.000 claims description 9
- 229940002612 prodrug Drugs 0.000 claims description 9
- 230000001965 increasing effect Effects 0.000 claims description 8
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 claims description 7
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 7
- 230000006870 function Effects 0.000 claims description 7
- 239000013563 matrix tablet Substances 0.000 claims description 7
- 238000002156 mixing Methods 0.000 claims description 7
- 206010001541 Akinesia Diseases 0.000 claims description 6
- 239000005557 antagonist Substances 0.000 claims description 6
- 229960004046 apomorphine Drugs 0.000 claims description 6
- 239000003543 catechol methyltransferase inhibitor Substances 0.000 claims description 6
- 238000003825 pressing Methods 0.000 claims description 6
- 206010006100 Bradykinesia Diseases 0.000 claims description 5
- 208000006083 Hypokinesia Diseases 0.000 claims description 5
- 206010044565 Tremor Diseases 0.000 claims description 5
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 5
- 229960004502 levodopa Drugs 0.000 claims description 5
- 239000003954 decarboxylase inhibitor Substances 0.000 claims description 4
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 4
- 230000000946 synaptic effect Effects 0.000 claims description 4
- 102100040999 Catechol O-methyltransferase Human genes 0.000 claims description 3
- 108020002739 Catechol O-methyltransferase Proteins 0.000 claims description 3
- 208000014094 Dystonic disease Diseases 0.000 claims description 3
- 102000010909 Monoamine Oxidase Human genes 0.000 claims description 3
- 108010062431 Monoamine oxidase Proteins 0.000 claims description 3
- 102000004257 Potassium Channel Human genes 0.000 claims description 3
- 239000000935 antidepressant agent Substances 0.000 claims description 3
- 229940005513 antidepressants Drugs 0.000 claims description 3
- 239000002111 antiemetic agent Substances 0.000 claims description 3
- 210000004227 basal ganglia Anatomy 0.000 claims description 3
- 229960004205 carbidopa Drugs 0.000 claims description 3
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical group NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims description 3
- 230000004064 dysfunction Effects 0.000 claims description 3
- 208000010118 dystonia Diseases 0.000 claims description 3
- 229960003337 entacapone Drugs 0.000 claims description 3
- JRURYQJSLYLRLN-BJMVGYQFSA-N entacapone Chemical compound CCN(CC)C(=O)C(\C#N)=C\C1=CC(O)=C(O)C([N+]([O-])=O)=C1 JRURYQJSLYLRLN-BJMVGYQFSA-N 0.000 claims description 3
- 230000001537 neural effect Effects 0.000 claims description 3
- 108020001213 potassium channel Proteins 0.000 claims description 3
- 230000002035 prolonged effect Effects 0.000 claims description 3
- 229960004603 tolcapone Drugs 0.000 claims description 3
- MIQPIUSUKVNLNT-UHFFFAOYSA-N tolcapone Chemical group C1=CC(C)=CC=C1C(=O)C1=CC(O)=C(O)C([N+]([O-])=O)=C1 MIQPIUSUKVNLNT-UHFFFAOYSA-N 0.000 claims description 3
- OQDPVLVUJFGPGQ-UHFFFAOYSA-N 2-[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl]pyrimidine Chemical compound C=1C=C2OCOC2=CC=1CN(CC1)CCN1C1=NC=CC=N1 OQDPVLVUJFGPGQ-UHFFFAOYSA-N 0.000 claims description 2
- 206010003591 Ataxia Diseases 0.000 claims description 2
- 102000007371 Ataxin-3 Human genes 0.000 claims description 2
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 claims description 2
- 206010008748 Chorea Diseases 0.000 claims description 2
- 229940123736 Decarboxylase inhibitor Drugs 0.000 claims description 2
- 239000003691 GABA modulator Substances 0.000 claims description 2
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 2
- 102000018899 Glutamate Receptors Human genes 0.000 claims description 2
- 108010027915 Glutamate Receptors Proteins 0.000 claims description 2
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 claims description 2
- 208000002569 Machado-Joseph Disease Diseases 0.000 claims description 2
- 208000002033 Myoclonus Diseases 0.000 claims description 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims description 2
- JUUFBMODXQKSTD-UHFFFAOYSA-N N-[2-amino-6-[(4-fluorophenyl)methylamino]-3-pyridinyl]carbamic acid ethyl ester Chemical group N1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 JUUFBMODXQKSTD-UHFFFAOYSA-N 0.000 claims description 2
- 208000005793 Restless legs syndrome Diseases 0.000 claims description 2
- 208000006289 Rett Syndrome Diseases 0.000 claims description 2
- 208000036834 Spinocerebellar ataxia type 3 Diseases 0.000 claims description 2
- 206010044074 Torticollis Diseases 0.000 claims description 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 2
- 208000016620 Tourette disease Diseases 0.000 claims description 2
- 208000018839 Wilson disease Diseases 0.000 claims description 2
- 230000003474 anti-emetic effect Effects 0.000 claims description 2
- 229960002802 bromocriptine Drugs 0.000 claims description 2
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical group C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims description 2
- 229960004596 cabergoline Drugs 0.000 claims description 2
- 208000012601 choreatic disease Diseases 0.000 claims description 2
- PCOBBVZJEWWZFR-UHFFFAOYSA-N ezogabine Chemical compound C1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 PCOBBVZJEWWZFR-UHFFFAOYSA-N 0.000 claims description 2
- 229960003667 flupirtine Drugs 0.000 claims description 2
- 208000036260 idiopathic disease Diseases 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 208000018197 inherited torticollis Diseases 0.000 claims description 2
- 102000048260 kappa Opioid Receptors Human genes 0.000 claims description 2
- XGZZHZMWIXFATA-UEZBDDGYSA-N nalfurafine Chemical group C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@H]3N(C)C(=O)\C=C\C1=COC=C1)CN2CC1CC1 XGZZHZMWIXFATA-UEZBDDGYSA-N 0.000 claims description 2
- 229960000441 nalfurafine Drugs 0.000 claims description 2
- 229960004310 piribedil Drugs 0.000 claims description 2
- RUOKEQAAGRXIBM-GFCCVEGCSA-N rasagiline Chemical compound C1=CC=C2[C@H](NCC#C)CCC2=C1 RUOKEQAAGRXIBM-GFCCVEGCSA-N 0.000 claims description 2
- 229960000245 rasagiline Drugs 0.000 claims description 2
- 229960003312 retigabine Drugs 0.000 claims description 2
- 230000001148 spastic effect Effects 0.000 claims description 2
- 108020001588 κ-opioid receptors Proteins 0.000 claims description 2
- 230000000561 anti-psychotic effect Effects 0.000 claims 2
- 229940098778 Dopamine receptor agonist Drugs 0.000 claims 1
- 208000026350 Inborn Genetic disease Diseases 0.000 claims 1
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 claims 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 1
- 230000001430 anti-depressive effect Effects 0.000 claims 1
- 208000016361 genetic disease Diseases 0.000 claims 1
- 239000002632 kappa opiate receptor agonist Substances 0.000 claims 1
- 229940126470 kappa opioid receptor agonist Drugs 0.000 claims 1
- 229960003587 lisuride Drugs 0.000 claims 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 1
- 229960003089 pramipexole Drugs 0.000 claims 1
- FASDKYOPVNHBLU-ZETCQYMHSA-N pramipexole Chemical compound C1[C@@H](NCCC)CCC2=C1SC(N)=N2 FASDKYOPVNHBLU-ZETCQYMHSA-N 0.000 claims 1
- 229960001879 ropinirole Drugs 0.000 claims 1
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 claims 1
- 239000002356 single layer Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 39
- ULSDMUVEXKOYBU-ZDUSSCGKSA-N zolmitriptan Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1C[C@H]1COC(=O)N1 ULSDMUVEXKOYBU-ZDUSSCGKSA-N 0.000 description 157
- 238000012360 testing method Methods 0.000 description 90
- 241000700159 Rattus Species 0.000 description 41
- ZISSAWUMDACLOM-UHFFFAOYSA-N triptane Chemical compound CC(C)C(C)(C)C ZISSAWUMDACLOM-UHFFFAOYSA-N 0.000 description 38
- 229950000505 tandospirone Drugs 0.000 description 32
- CEIJFEGBUDEYSX-FZDBZEDMSA-N tandospirone Chemical compound O=C([C@@H]1[C@H]2CC[C@H](C2)[C@@H]1C1=O)N1CCCCN(CC1)CCN1C1=NC=CC=N1 CEIJFEGBUDEYSX-FZDBZEDMSA-N 0.000 description 32
- 241001465754 Metazoa Species 0.000 description 30
- 238000000034 method Methods 0.000 description 30
- 150000001875 compounds Chemical class 0.000 description 28
- -1 for example Chemical compound 0.000 description 25
- 238000004090 dissolution Methods 0.000 description 23
- DIVDFFZHCJEHGG-UHFFFAOYSA-N oxidopamine Chemical compound NCCC1=CC(O)=C(O)C=C1O DIVDFFZHCJEHGG-UHFFFAOYSA-N 0.000 description 22
- 235000012222 talc Nutrition 0.000 description 22
- 229940033134 talc Drugs 0.000 description 22
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 20
- 239000000243 solution Substances 0.000 description 20
- 238000013270 controlled release Methods 0.000 description 19
- 239000007924 injection Substances 0.000 description 19
- 238000002347 injection Methods 0.000 description 19
- 230000036470 plasma concentration Effects 0.000 description 17
- 239000002552 dosage form Substances 0.000 description 15
- 230000008569 process Effects 0.000 description 14
- 230000002829 reductive effect Effects 0.000 description 14
- ULFRLSNUDGIQQP-UHFFFAOYSA-N rizatriptan Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1CN1C=NC=N1 ULFRLSNUDGIQQP-UHFFFAOYSA-N 0.000 description 14
- 230000004913 activation Effects 0.000 description 13
- 238000011161 development Methods 0.000 description 13
- 238000005469 granulation Methods 0.000 description 13
- 230000003179 granulation Effects 0.000 description 13
- 229960000425 rizatriptan Drugs 0.000 description 13
- 229920001661 Chitosan Polymers 0.000 description 12
- 239000002775 capsule Substances 0.000 description 12
- 238000007877 drug screening Methods 0.000 description 11
- 229940068196 placebo Drugs 0.000 description 11
- 239000000902 placebo Substances 0.000 description 11
- 239000000047 product Substances 0.000 description 11
- 238000011552 rat model Methods 0.000 description 11
- 231100000915 pathological change Toxicity 0.000 description 10
- 230000036285 pathological change Effects 0.000 description 10
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- 238000004458 analytical method Methods 0.000 description 9
- 230000009286 beneficial effect Effects 0.000 description 9
- 239000003795 chemical substances by application Substances 0.000 description 9
- 238000004519 manufacturing process Methods 0.000 description 9
- AMKVXSZCKVJAGH-UHFFFAOYSA-N naratriptan Chemical compound C12=CC(CCS(=O)(=O)NC)=CC=C2NC=C1C1CCN(C)CC1 AMKVXSZCKVJAGH-UHFFFAOYSA-N 0.000 description 9
- WKEMJKQOLOHJLZ-UHFFFAOYSA-N Almogran Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1CS(=O)(=O)N1CCCC1 WKEMJKQOLOHJLZ-UHFFFAOYSA-N 0.000 description 8
- DLRVVLDZNNYCBX-UHFFFAOYSA-N Polydextrose Polymers OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(O)O1 DLRVVLDZNNYCBX-UHFFFAOYSA-N 0.000 description 8
- 238000010521 absorption reaction Methods 0.000 description 8
- PKZXLMVXBZICTF-UHFFFAOYSA-N befiradol Chemical compound N1=CC(C)=CC=C1CNCC1(F)CCN(C(=O)C=2C=C(Cl)C(F)=CC=2)CC1 PKZXLMVXBZICTF-UHFFFAOYSA-N 0.000 description 8
- 239000011230 binding agent Substances 0.000 description 8
- 230000000875 corresponding effect Effects 0.000 description 8
- 208000035475 disorder Diseases 0.000 description 8
- PWVXXGRKLHYWKM-LJQANCHMSA-N eletriptan Chemical compound CN1CCC[C@@H]1CC(C1=C2)=CNC1=CC=C2CCS(=O)(=O)C1=CC=CC=C1 PWVXXGRKLHYWKM-LJQANCHMSA-N 0.000 description 8
- 238000011156 evaluation Methods 0.000 description 8
- 229960002284 frovatriptan Drugs 0.000 description 8
- SIBNYOSJIXCDRI-SECBINFHSA-N frovatriptan Chemical compound C1=C(C(N)=O)[CH]C2=C(C[C@H](NC)CC3)C3=NC2=C1 SIBNYOSJIXCDRI-SECBINFHSA-N 0.000 description 8
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 8
- 229960005254 naratriptan Drugs 0.000 description 8
- 238000005507 spraying Methods 0.000 description 8
- KQKPFRSPSRPDEB-UHFFFAOYSA-N sumatriptan Chemical compound CNS(=O)(=O)CC1=CC=C2NC=C(CCN(C)C)C2=C1 KQKPFRSPSRPDEB-UHFFFAOYSA-N 0.000 description 8
- 230000009471 action Effects 0.000 description 7
- 229960002133 almotriptan Drugs 0.000 description 7
- 229950007200 befiradol Drugs 0.000 description 7
- 229960002472 eletriptan Drugs 0.000 description 7
- 239000000945 filler Substances 0.000 description 7
- PPRRDFIXUUSXRA-UHFFFAOYSA-N flibanserin Chemical compound FC(F)(F)C1=CC=CC(N2CCN(CCN3C(NC4=CC=CC=C43)=O)CC2)=C1 PPRRDFIXUUSXRA-UHFFFAOYSA-N 0.000 description 7
- QOIGKGMMAGJZNZ-UHFFFAOYSA-N gepirone Chemical compound O=C1CC(C)(C)CC(=O)N1CCCCN1CCN(C=2N=CC=CN=2)CC1 QOIGKGMMAGJZNZ-UHFFFAOYSA-N 0.000 description 7
- 230000003902 lesion Effects 0.000 description 7
- YGYBFMRFXNDIPO-QGZVFWFLSA-N repinotan Chemical compound O=S1(=O)C2=CC=CC=C2C(=O)N1CCCCNC[C@@H]1OC2=CC=CC=C2CC1 YGYBFMRFXNDIPO-QGZVFWFLSA-N 0.000 description 7
- 229950009693 repinotan Drugs 0.000 description 7
- 229960003708 sumatriptan Drugs 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- 230000002195 synergetic effect Effects 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- BVMYCHKQPGEOSI-UHFFFAOYSA-N 8-[2-(2,3-dihydro-1,4-benzodioxin-3-ylmethylamino)ethyl]-8-azaspiro[4.5]decane-7,9-dione Chemical compound C1C(=O)N(CCNCC2OC3=CC=CC=C3OC2)C(=O)CC21CCCC2 BVMYCHKQPGEOSI-UHFFFAOYSA-N 0.000 description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 6
- 206010040108 Serotonin syndrome Diseases 0.000 description 6
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 6
- 210000004556 brain Anatomy 0.000 description 6
- 229940000425 combination drug Drugs 0.000 description 6
- 239000013066 combination product Substances 0.000 description 6
- 239000008121 dextrose Substances 0.000 description 6
- 229960002053 flibanserin Drugs 0.000 description 6
- 229960000647 gepirone Drugs 0.000 description 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 6
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 6
- 229960003943 hypromellose Drugs 0.000 description 6
- 230000002197 limbic effect Effects 0.000 description 6
- 230000007774 longterm Effects 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- 229940076279 serotonin Drugs 0.000 description 6
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 5
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 5
- 102000035038 5-HT1 receptors Human genes 0.000 description 5
- 108091005478 5-HT1 receptors Proteins 0.000 description 5
- QYFHCFNBYQZGKW-BDQAORGHSA-N 8-[4-[[(3s)-5-methoxy-3,4-dihydro-2h-chromen-3-yl]-propylamino]butyl]-8-azaspiro[4.5]decane-7,9-dione;hydrochloride Chemical compound Cl.CCCN([C@H]1CC2=C(OC)C=CC=C2OC1)CCCCN(C(C1)=O)C(=O)CC21CCCC2 QYFHCFNBYQZGKW-BDQAORGHSA-N 0.000 description 5
- 241000282693 Cercopithecidae Species 0.000 description 5
- 239000001856 Ethyl cellulose Substances 0.000 description 5
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 5
- 229920003091 Methocel™ Polymers 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 229920002472 Starch Polymers 0.000 description 5
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 5
- 235000010443 alginic acid Nutrition 0.000 description 5
- 229920000615 alginic acid Polymers 0.000 description 5
- 229950000420 alnespirone Drugs 0.000 description 5
- 238000010171 animal model Methods 0.000 description 5
- 229950005615 binospirone Drugs 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 230000007423 decrease Effects 0.000 description 5
- 230000000632 dystonic effect Effects 0.000 description 5
- 235000019325 ethyl cellulose Nutrition 0.000 description 5
- 229920001249 ethyl cellulose Polymers 0.000 description 5
- 235000013305 food Nutrition 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 239000000314 lubricant Substances 0.000 description 5
- 229920000609 methyl cellulose Polymers 0.000 description 5
- 235000010981 methylcellulose Nutrition 0.000 description 5
- 239000001923 methylcellulose Substances 0.000 description 5
- 229960002900 methylcellulose Drugs 0.000 description 5
- 210000003205 muscle Anatomy 0.000 description 5
- 210000002569 neuron Anatomy 0.000 description 5
- URMTUEWUIGOJBW-UHFFFAOYSA-N piclozotan Chemical compound ClC1=COC2=CC=CC=C2C(=O)N1CCCCN(CC=1)CCC=1C1=CC=CC=N1 URMTUEWUIGOJBW-UHFFFAOYSA-N 0.000 description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 5
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 5
- 239000002243 precursor Substances 0.000 description 5
- 239000003521 serotonin 5-HT1 receptor agonist Substances 0.000 description 5
- 235000010413 sodium alginate Nutrition 0.000 description 5
- 239000000661 sodium alginate Substances 0.000 description 5
- 229940005550 sodium alginate Drugs 0.000 description 5
- 239000007787 solid Substances 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- 229940032147 starch Drugs 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- 239000008107 starch Substances 0.000 description 5
- 238000007920 subcutaneous administration Methods 0.000 description 5
- 230000005062 synaptic transmission Effects 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 4
- FBVFZWUMDDXLLG-HDICACEKSA-N (3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)-1-piperazinyl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione Chemical compound C1=CC=C2C(N3CCN(CC3)CCCCN3C(=O)[C@@H]4CCCC[C@@H]4C3=O)=NSC2=C1 FBVFZWUMDDXLLG-HDICACEKSA-N 0.000 description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 4
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 229920002307 Dextran Polymers 0.000 description 4
- 239000004375 Dextrin Substances 0.000 description 4
- 229920001353 Dextrin Polymers 0.000 description 4
- 229920002774 Maltodextrin Polymers 0.000 description 4
- 239000005913 Maltodextrin Substances 0.000 description 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 4
- 229920001100 Polydextrose Polymers 0.000 description 4
- 241000283984 Rodentia Species 0.000 description 4
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 4
- 239000000164 antipsychotic agent Substances 0.000 description 4
- 230000033228 biological regulation Effects 0.000 description 4
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 235000010980 cellulose Nutrition 0.000 description 4
- 229920002678 cellulose Polymers 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
- 230000003111 delayed effect Effects 0.000 description 4
- 235000019425 dextrin Nutrition 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 235000019253 formic acid Nutrition 0.000 description 4
- 230000001771 impaired effect Effects 0.000 description 4
- 230000014759 maintenance of location Effects 0.000 description 4
- 229940035034 maltodextrin Drugs 0.000 description 4
- 239000012528 membrane Substances 0.000 description 4
- 239000002858 neurotransmitter agent Substances 0.000 description 4
- 229960002748 norepinephrine Drugs 0.000 description 4
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 4
- 229950002181 piclozotan Drugs 0.000 description 4
- 235000013856 polydextrose Nutrition 0.000 description 4
- 239000001259 polydextrose Substances 0.000 description 4
- 229940035035 polydextrose Drugs 0.000 description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 4
- 229920000053 polysorbate 80 Polymers 0.000 description 4
- 238000012216 screening Methods 0.000 description 4
- 239000000952 serotonin receptor agonist Substances 0.000 description 4
- 239000007921 spray Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 239000007929 subcutaneous injection Substances 0.000 description 4
- 238000010254 subcutaneous injection Methods 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 231100001274 therapeutic index Toxicity 0.000 description 4
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 description 3
- TZJUVVIWVWFLCD-UHFFFAOYSA-N 1,1-dioxo-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,2-benzothiazol-3-one Chemical compound O=S1(=O)C2=CC=CC=C2C(=O)N1CCCCN(CC1)CCN1C1=NC=CC=N1 TZJUVVIWVWFLCD-UHFFFAOYSA-N 0.000 description 3
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 229920002907 Guar gum Polymers 0.000 description 3
- 241000282414 Homo sapiens Species 0.000 description 3
- 241000282553 Macaca Species 0.000 description 3
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- 229930006000 Sucrose Natural products 0.000 description 3
- 206010043118 Tardive Dyskinesia Diseases 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 230000003213 activating effect Effects 0.000 description 3
- 239000000783 alginic acid Substances 0.000 description 3
- 229960001126 alginic acid Drugs 0.000 description 3
- 150000004781 alginic acids Chemical class 0.000 description 3
- 229940025084 amphetamine Drugs 0.000 description 3
- 238000000540 analysis of variance Methods 0.000 description 3
- 230000001174 ascending effect Effects 0.000 description 3
- 235000010418 carrageenan Nutrition 0.000 description 3
- 239000000679 carrageenan Substances 0.000 description 3
- 229920001525 carrageenan Polymers 0.000 description 3
- 229940113118 carrageenan Drugs 0.000 description 3
- 229920002301 cellulose acetate Polymers 0.000 description 3
- 230000001055 chewing effect Effects 0.000 description 3
- 238000009826 distribution Methods 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 239000008273 gelatin Substances 0.000 description 3
- 229920000159 gelatin Polymers 0.000 description 3
- 235000019322 gelatine Nutrition 0.000 description 3
- 235000011852 gelatine desserts Nutrition 0.000 description 3
- 229940049654 glyceryl behenate Drugs 0.000 description 3
- 235000010417 guar gum Nutrition 0.000 description 3
- 239000000665 guar gum Substances 0.000 description 3
- 229960002154 guar gum Drugs 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 239000008172 hydrogenated vegetable oil Substances 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 229950003599 ipsapirone Drugs 0.000 description 3
- 239000004031 partial agonist Substances 0.000 description 3
- 239000008188 pellet Substances 0.000 description 3
- 229950004193 perospirone Drugs 0.000 description 3
- 239000008363 phosphate buffer Substances 0.000 description 3
- 229920001223 polyethylene glycol Polymers 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 230000036544 posture Effects 0.000 description 3
- 229940069328 povidone Drugs 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- 238000011002 quantification Methods 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 230000004044 response Effects 0.000 description 3
- HKFMQJUJWSFOLY-OAQYLSRUSA-N sarizotan Chemical group C1=CC(F)=CC=C1C1=CN=CC(CNC[C@@H]2OC3=CC=CC=C3CC2)=C1 HKFMQJUJWSFOLY-OAQYLSRUSA-N 0.000 description 3
- 230000000862 serotonergic effect Effects 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 238000013222 sprague-dawley male rat Methods 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 210000000225 synapse Anatomy 0.000 description 3
- 238000011269 treatment regimen Methods 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 3
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 2
- 229930182837 (R)-adrenaline Natural products 0.000 description 2
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 description 2
- SGUAFYQXFOLMHL-UHFFFAOYSA-N 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide Chemical compound C=1C=C(O)C(C(N)=O)=CC=1C(O)CNC(C)CCC1=CC=CC=C1 SGUAFYQXFOLMHL-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- 208000019901 Anxiety disease Diseases 0.000 description 2
- 102100038238 Aromatic-L-amino-acid decarboxylase Human genes 0.000 description 2
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
- 229930091371 Fructose Natural products 0.000 description 2
- 239000005715 Fructose Substances 0.000 description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 2
- 229920000084 Gum arabic Polymers 0.000 description 2
- 101150015707 HTR1A gene Proteins 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229920003102 Methocel™ E4M Polymers 0.000 description 2
- 208000019695 Migraine disease Diseases 0.000 description 2
- 101710138657 Neurotoxin Proteins 0.000 description 2
- 208000027089 Parkinsonian disease Diseases 0.000 description 2
- 206010034010 Parkinsonism Diseases 0.000 description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- 108010035075 Tyrosine decarboxylase Proteins 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- 235000010489 acacia gum Nutrition 0.000 description 2
- 239000000205 acacia gum Substances 0.000 description 2
- 150000003863 ammonium salts Chemical class 0.000 description 2
- 230000003542 behavioural effect Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 229960001768 buspirone hydrochloride Drugs 0.000 description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- 235000010216 calcium carbonate Nutrition 0.000 description 2
- 239000001506 calcium phosphate Substances 0.000 description 2
- 229910000389 calcium phosphate Inorganic materials 0.000 description 2
- 235000011010 calcium phosphates Nutrition 0.000 description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
- 235000013539 calcium stearate Nutrition 0.000 description 2
- 239000008116 calcium stearate Substances 0.000 description 2
- 235000011132 calcium sulphate Nutrition 0.000 description 2
- 229960001631 carbomer Drugs 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
- 235000019438 castor oil Nutrition 0.000 description 2
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 2
- 238000005119 centrifugation Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 230000002301 combined effect Effects 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 230000001276 controlling effect Effects 0.000 description 2
- 230000002596 correlated effect Effects 0.000 description 2
- 230000007850 degeneration Effects 0.000 description 2
- 210000002455 dental arch Anatomy 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000007884 disintegrant Substances 0.000 description 2
- 239000003210 dopamine receptor blocking agent Substances 0.000 description 2
- 210000005064 dopaminergic neuron Anatomy 0.000 description 2
- 239000003651 drinking water Substances 0.000 description 2
- 235000020188 drinking water Nutrition 0.000 description 2
- 238000009506 drug dissolution testing Methods 0.000 description 2
- 230000008030 elimination Effects 0.000 description 2
- 238000003379 elimination reaction Methods 0.000 description 2
- WVLHGCRWEHCIOT-UHFFFAOYSA-N eltoprazine Chemical compound C1CNCCN1C1=CC=CC2=C1OCCO2 WVLHGCRWEHCIOT-UHFFFAOYSA-N 0.000 description 2
- 229950006047 eltoprazine Drugs 0.000 description 2
- 230000007613 environmental effect Effects 0.000 description 2
- 229960005139 epinephrine Drugs 0.000 description 2
- 239000011152 fibreglass Substances 0.000 description 2
- NYSDRDDQELAVKP-SFHVURJKSA-N flesinoxan Chemical compound C([C@@H](O1)CO)OC2=C1C=CC=C2N(CC1)CCN1CCNC(=O)C1=CC=C(F)C=C1 NYSDRDDQELAVKP-SFHVURJKSA-N 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 2
- LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 239000001341 hydroxy propyl starch Substances 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
- 235000013828 hydroxypropyl starch Nutrition 0.000 description 2
- 229940071676 hydroxypropylcellulose Drugs 0.000 description 2
- 230000001660 hyperkinetic effect Effects 0.000 description 2
- 238000011065 in-situ storage Methods 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- 239000000905 isomalt Substances 0.000 description 2
- 235000010439 isomalt Nutrition 0.000 description 2
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 description 2
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 2
- 210000001847 jaw Anatomy 0.000 description 2
- 229960001632 labetalol Drugs 0.000 description 2
- 239000000832 lactitol Substances 0.000 description 2
- 235000010448 lactitol Nutrition 0.000 description 2
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 2
- 229960003451 lactitol Drugs 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 238000004811 liquid chromatography Methods 0.000 description 2
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- 238000011866 long-term treatment Methods 0.000 description 2
- 230000001050 lubricating effect Effects 0.000 description 2
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 2
- 239000000395 magnesium oxide Substances 0.000 description 2
- 229960000869 magnesium oxide Drugs 0.000 description 2
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 2
- 238000012423 maintenance Methods 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 230000007721 medicinal effect Effects 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- XBBDACCLCFWBSI-ZETCQYMHSA-N melevodopa Chemical compound COC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 XBBDACCLCFWBSI-ZETCQYMHSA-N 0.000 description 2
- 229960001794 melevodopa Drugs 0.000 description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 206010027599 migraine Diseases 0.000 description 2
- 239000002581 neurotoxin Substances 0.000 description 2
- 231100000618 neurotoxin Toxicity 0.000 description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- MEEQBDCQPIZMLY-HNNXBMFYSA-N osemozotan Chemical compound C1=C2OCOC2=CC(OCCCNC[C@@H]2OC3=CC=CC=C3OC2)=C1 MEEQBDCQPIZMLY-HNNXBMFYSA-N 0.000 description 2
- 230000036961 partial effect Effects 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 229960000502 poloxamer Drugs 0.000 description 2
- 229920001983 poloxamer Polymers 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 230000008092 positive effect Effects 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 238000011045 prefiltration Methods 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000005070 sampling Methods 0.000 description 2
- 229950007903 sarizotan Drugs 0.000 description 2
- 229910052710 silicon Inorganic materials 0.000 description 2
- 239000010703 silicon Substances 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 2
- 235000010356 sorbitol Nutrition 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 229960002920 sorbitol Drugs 0.000 description 2
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 229960004274 stearic acid Drugs 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- 239000007939 sustained release tablet Substances 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 238000004885 tandem mass spectrometry Methods 0.000 description 2
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 2
- APJYDQYYACXCRM-UHFFFAOYSA-N tryptamine Chemical compound C1=CC=C2C(CCN)=CNC2=C1 APJYDQYYACXCRM-UHFFFAOYSA-N 0.000 description 2
- 210000001364 upper extremity Anatomy 0.000 description 2
- 239000003643 water by type Substances 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
- 235000010447 xylitol Nutrition 0.000 description 2
- 229960002675 xylitol Drugs 0.000 description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 2
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 2
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 1
- JLHMJWHSBYZWJJ-UHFFFAOYSA-N 1,2-thiazole 1-oxide Chemical compound O=S1C=CC=N1 JLHMJWHSBYZWJJ-UHFFFAOYSA-N 0.000 description 1
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 description 1
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 description 1
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 description 1
- 102100036312 5-hydroxytryptamine receptor 1E Human genes 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 206010001540 Akathisia Diseases 0.000 description 1
- USFZMSVCRYTOJT-UHFFFAOYSA-N Ammonium acetate Chemical compound N.CC(O)=O USFZMSVCRYTOJT-UHFFFAOYSA-N 0.000 description 1
- 239000005695 Ammonium acetate Substances 0.000 description 1
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 description 1
- 102000003823 Aromatic-L-amino-acid decarboxylases Human genes 0.000 description 1
- 108090000121 Aromatic-L-amino-acid decarboxylases Proteins 0.000 description 1
- 208000012219 Autonomic Nervous System disease Diseases 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 206010010071 Coma Diseases 0.000 description 1
- 208000034656 Contusions Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 235000010919 Copernicia prunifera Nutrition 0.000 description 1
- 244000180278 Copernicia prunifera Species 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 102000015554 Dopamine receptor Human genes 0.000 description 1
- 108050004812 Dopamine receptor Proteins 0.000 description 1
- 229940121891 Dopamine receptor antagonist Drugs 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 239000001116 FEMA 4028 Substances 0.000 description 1
- 230000005526 G1 to G0 transition Effects 0.000 description 1
- 206010017577 Gait disturbance Diseases 0.000 description 1
- 101150004776 HTR1E gene Proteins 0.000 description 1
- 101150104779 HTR2A gene Proteins 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- 208000008454 Hyperhidrosis Diseases 0.000 description 1
- 208000000269 Hyperkinesis Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 208000015592 Involuntary movements Diseases 0.000 description 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 208000002740 Muscle Rigidity Diseases 0.000 description 1
- 206010028347 Muscle twitching Diseases 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- CEIJFEGBUDEYSX-USTZCAOPSA-N O=C([C@@H]1[C@H](C2=O)[C@]3([H])CC[C@]1(C3)[H])N2CCCCN(CC1)CCN1C1=NC=CC=N1 Chemical compound O=C([C@@H]1[C@H](C2=O)[C@]3([H])CC[C@]1(C3)[H])N2CCCCN(CC1)CCN1C1=NC=CC=N1 CEIJFEGBUDEYSX-USTZCAOPSA-N 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 229920005439 Perspex® Polymers 0.000 description 1
- 241000233805 Phoenix Species 0.000 description 1
- 208000005374 Poisoning Diseases 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 238000012356 Product development Methods 0.000 description 1
- 208000001431 Psychomotor Agitation Diseases 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229910000831 Steel Inorganic materials 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- 238000003639 Student–Newman–Keuls (SNK) method Methods 0.000 description 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 1
- 229920002494 Zein Polymers 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 description 1
- GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 229940023476 agar Drugs 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- WOLHOYHSEKDWQH-UHFFFAOYSA-N amantadine hydrochloride Chemical compound [Cl-].C1C(C2)CC3CC2CC1([NH3+])C3 WOLHOYHSEKDWQH-UHFFFAOYSA-N 0.000 description 1
- 229960003036 amisulpride Drugs 0.000 description 1
- NTJOBXMMWNYJFB-UHFFFAOYSA-N amisulpride Chemical compound CCN1CCCC1CNC(=O)C1=CC(S(=O)(=O)CC)=C(N)C=C1OC NTJOBXMMWNYJFB-UHFFFAOYSA-N 0.000 description 1
- 229940043376 ammonium acetate Drugs 0.000 description 1
- 235000019257 ammonium acetate Nutrition 0.000 description 1
- 230000000181 anti-adherent effect Effects 0.000 description 1
- 229940125683 antiemetic agent Drugs 0.000 description 1
- 229940005529 antipsychotics Drugs 0.000 description 1
- CXWQXGNFZLHLHQ-DPFCLETOSA-N apomorphine hydrochloride Chemical compound [H+].[H+].O.[Cl-].[Cl-].C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3.C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 CXWQXGNFZLHLHQ-DPFCLETOSA-N 0.000 description 1
- 229960004372 aripiprazole Drugs 0.000 description 1
- 210000003403 autonomic nervous system Anatomy 0.000 description 1
- 229940125717 barbiturate Drugs 0.000 description 1
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 1
- 229960004853 betadex Drugs 0.000 description 1
- 230000008512 biological response Effects 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 238000004820 blood count Methods 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 229960005069 calcium Drugs 0.000 description 1
- 235000001465 calcium Nutrition 0.000 description 1
- 235000010410 calcium alginate Nutrition 0.000 description 1
- 239000000648 calcium alginate Substances 0.000 description 1
- 229960002681 calcium alginate Drugs 0.000 description 1
- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 210000001715 carotid artery Anatomy 0.000 description 1
- 150000003943 catecholamines Chemical class 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 229940045110 chitosan Drugs 0.000 description 1
- 238000013375 chromatographic separation Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 239000000306 component Substances 0.000 description 1
- 230000036461 convulsion Effects 0.000 description 1
- 239000012792 core layer Substances 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- WTVNFKVGGUWHQC-UHFFFAOYSA-N decane-2,4-dione Chemical compound CCCCCCC(=O)CC(C)=O WTVNFKVGGUWHQC-UHFFFAOYSA-N 0.000 description 1
- 238000006114 decarboxylation reaction Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000003412 degenerative effect Effects 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000010432 diamond Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000006073 displacement reaction Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 description 1
- 229940043264 dodecyl sulfate Drugs 0.000 description 1
- 229960000394 droperidol Drugs 0.000 description 1
- RMEDXOLNCUSCGS-UHFFFAOYSA-N droperidol Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CC=C(N2C(NC3=CC=CC=C32)=O)CC1 RMEDXOLNCUSCGS-UHFFFAOYSA-N 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000000074 effect on parkinson Effects 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 210000003238 esophagus Anatomy 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 210000003414 extremity Anatomy 0.000 description 1
- 238000000556 factor analysis Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 229950003678 flesinoxan Drugs 0.000 description 1
- 229960002464 fluoxetine Drugs 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 210000003194 forelimb Anatomy 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 description 1
- 229940046813 glyceryl palmitostearate Drugs 0.000 description 1
- 230000005484 gravity Effects 0.000 description 1
- 208000035474 group of disease Diseases 0.000 description 1
- 229960003878 haloperidol Drugs 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 230000033444 hydroxylation Effects 0.000 description 1
- 238000005805 hydroxylation reaction Methods 0.000 description 1
- 206010020745 hyperreflexia Diseases 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 208000018879 impaired coordination Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000013067 intermediate product Substances 0.000 description 1
- 238000001361 intraarterial administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 210000000265 leukocyte Anatomy 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229940037627 magnesium lauryl sulfate Drugs 0.000 description 1
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000012907 medicinal substance Substances 0.000 description 1
- 229960003987 melatonin Drugs 0.000 description 1
- DRLFMBDRBRZALE-UHFFFAOYSA-N melatonin Chemical compound COC1=CC=C2NC=C(CCNC(C)=O)C2=C1 DRLFMBDRBRZALE-UHFFFAOYSA-N 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- 229960004503 metoclopramide Drugs 0.000 description 1
- TTWJBBZEZQICBI-UHFFFAOYSA-N metoclopramide Chemical compound CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC TTWJBBZEZQICBI-UHFFFAOYSA-N 0.000 description 1
- 239000004005 microsphere Substances 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
- 230000037023 motor activity Effects 0.000 description 1
- 230000004118 muscle contraction Effects 0.000 description 1
- 230000003387 muscular Effects 0.000 description 1
- 230000017311 musculoskeletal movement, spinal reflex action Effects 0.000 description 1
- IXRNQIKIVWWFBH-UHFFFAOYSA-N n-(1-phenylethenyl)acetamide Chemical compound CC(=O)NC(=C)C1=CC=CC=C1 IXRNQIKIVWWFBH-UHFFFAOYSA-N 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 230000009251 neurologic dysfunction Effects 0.000 description 1
- 208000015015 neurological dysfunction Diseases 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 208000018360 neuromuscular disease Diseases 0.000 description 1
- WBQQSAGCMDCEJG-UHFFFAOYSA-N nona-4,6,8-trien-3-one Chemical compound CCC(C=CC=CC=C)=O WBQQSAGCMDCEJG-UHFFFAOYSA-N 0.000 description 1
- 230000002474 noradrenergic effect Effects 0.000 description 1
- 238000001543 one-way ANOVA Methods 0.000 description 1
- 229940005483 opioid analgesics Drugs 0.000 description 1
- 229940100691 oral capsule Drugs 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 239000007935 oral tablet Substances 0.000 description 1
- 229940096978 oral tablet Drugs 0.000 description 1
- 229950003614 osemozotan Drugs 0.000 description 1
- 208000021090 palsy Diseases 0.000 description 1
- 230000001314 paroxysmal effect Effects 0.000 description 1
- 229960001412 pentobarbital Drugs 0.000 description 1
- WEXRUCMBJFQVBZ-UHFFFAOYSA-N pentobarbital Chemical compound CCCC(C)C1(CC)C(=O)NC(=O)NC1=O WEXRUCMBJFQVBZ-UHFFFAOYSA-N 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- YVUQSNJEYSNKRX-UHFFFAOYSA-N pimozide Chemical compound C1=CC(F)=CC=C1C(C=1C=CC(F)=CC=1)CCCN1CCC(N2C(NC3=CC=CC=C32)=O)CC1 YVUQSNJEYSNKRX-UHFFFAOYSA-N 0.000 description 1
- 229960003634 pimozide Drugs 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 229960005455 polacrilin Drugs 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 239000004926 polymethyl methacrylate Substances 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 230000001242 postsynaptic effect Effects 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- ZRHANBBTXQZFSP-UHFFFAOYSA-M potassium;4-amino-3,5,6-trichloropyridine-2-carboxylate Chemical compound [K+].NC1=C(Cl)C(Cl)=NC(C([O-])=O)=C1Cl ZRHANBBTXQZFSP-UHFFFAOYSA-M 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 210000005215 presynaptic neuron Anatomy 0.000 description 1
- 238000002203 pretreatment Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- WIKYUJGCLQQFNW-UHFFFAOYSA-N prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 description 1
- 229960003111 prochlorperazine Drugs 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 108700016586 rat AIM Proteins 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 229960001534 risperidone Drugs 0.000 description 1
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 description 1
- 229940004193 rizatriptan 10 mg Drugs 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000004002 serotonin 1B agonist Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229940023144 sodium glycolate Drugs 0.000 description 1
- 239000002594 sorbent Substances 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 238000004544 sputter deposition Methods 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000010959 steel Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
- 239000002700 tablet coating Substances 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000012956 testing procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- 229960003991 trazodone Drugs 0.000 description 1
- PHLBKPHSAVXXEF-UHFFFAOYSA-N trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 description 1
- ZEWQUBUPAILYHI-UHFFFAOYSA-N trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 description 1
- 229960002324 trifluoperazine Drugs 0.000 description 1
- JEJAMASKDTUEBZ-UHFFFAOYSA-N tris(1,1,3-tribromo-2,2-dimethylpropyl) phosphate Chemical compound BrCC(C)(C)C(Br)(Br)OP(=O)(OC(Br)(Br)C(C)(C)CBr)OC(Br)(Br)C(C)(C)CBr JEJAMASKDTUEBZ-UHFFFAOYSA-N 0.000 description 1
- 238000007473 univariate analysis Methods 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 229960004688 venlafaxine Drugs 0.000 description 1
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 230000021542 voluntary musculoskeletal movement Effects 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- 229940045860 white wax Drugs 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000005019 zein Substances 0.000 description 1
- 229940093612 zein Drugs 0.000 description 1
- 229940057977 zinc stearate Drugs 0.000 description 1
- 229960004141 zuclopenthixol Drugs 0.000 description 1
- WFPIAZLQTJBIFN-DVZOWYKESA-N zuclopenthixol Chemical compound C1CN(CCO)CCN1CC\C=C\1C2=CC(Cl)=CC=C2SC2=CC=CC=C2/1 WFPIAZLQTJBIFN-DVZOWYKESA-N 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Inorganic Chemistry (AREA)
- Psychology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201270196 | 2012-04-18 | ||
| DKPA201270196 | 2012-04-18 | ||
| PCT/DK2012/050190 WO2012163365A1 (en) | 2011-06-01 | 2012-06-01 | Combinations of serotonin receptor agonists for treatment of movement disorders |
| DKPCT/DK2012/050190 | 2012-06-01 | ||
| DKPA201270755 | 2012-12-04 | ||
| DKPA201270755 | 2012-12-04 | ||
| PCT/DK2013/050111 WO2013156035A1 (en) | 2012-04-18 | 2013-04-18 | Orally available pharmaceutical formulation suitable for improved management of movement disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2014145944A RU2014145944A (ru) | 2016-06-10 |
| RU2670272C2 true RU2670272C2 (ru) | 2018-10-22 |
Family
ID=49382938
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014145944A RU2670272C2 (ru) | 2012-04-18 | 2013-04-18 | Пероральная фармацевтическая композиция, подходящая для повышения эффективности лечения двигательных нарушений |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10561618B2 (cs) |
| EP (1) | EP2838517B1 (cs) |
| JP (1) | JP6216768B2 (cs) |
| KR (1) | KR102104635B1 (cs) |
| CN (1) | CN104411301B (cs) |
| AU (1) | AU2013248685B2 (cs) |
| BR (1) | BR112014025907B1 (cs) |
| CA (1) | CA2870123C (cs) |
| DK (1) | DK2838517T3 (cs) |
| ES (1) | ES2654787T3 (cs) |
| HU (1) | HUE037732T2 (cs) |
| IL (1) | IL235000B (cs) |
| IN (1) | IN2014DN09571A (cs) |
| MX (1) | MX361372B (cs) |
| MY (1) | MY169068A (cs) |
| NO (1) | NO2838517T3 (cs) |
| NZ (1) | NZ700474A (cs) |
| PH (1) | PH12014502331B1 (cs) |
| PL (1) | PL2838517T3 (cs) |
| PT (1) | PT2838517T (cs) |
| RU (1) | RU2670272C2 (cs) |
| SG (1) | SG11201406690SA (cs) |
| WO (1) | WO2013156035A1 (cs) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2813095C1 (ru) * | 2023-08-07 | 2024-02-06 | Непубличное акционерное общество "Северная звезда" | Фармацевтическая композиция, содержащая золмитриптан, и технология ее производства |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2950469C (en) * | 2014-06-26 | 2022-09-20 | Contera Pharma Aps | Use of buspirone metabolites |
| MX374938B (es) * | 2014-07-09 | 2025-03-06 | Pf Medicament | Un método para el tratamiento de trastornos del movimiento con befiradol. |
| BR112017015487A2 (pt) | 2015-01-20 | 2018-01-30 | Xoc Pharmaceuticals Inc | Composto; composição; método de tratamento e/ou prevenção de enxaqueca, als, doença de alzheimer, doença de parkinson, distúrbios extrapirimidais, depressão, náusea, êmese, síndrome das pernas inquietas, insônia, agressão, doença de huntington, doença cardiopulmonar, fibrogênese, hipertensão arterial pulmonar, ansiedade, dependências a drogas, distonia, parassonia ou hiperlactinemia em um indivíduo; métodos de agonização dos receptores d2, 5-ht1d, 5-ht1a e 5-ht2c, em um indivíduo; método de antagonização do receptor d3 em um indivíduo; métodos de agonização seletiva dos receptores 5 -ht1d, e 5-ht2c, método de fornecimento de atividade de antagonista funcional no receptor 5 -ht2b ou no receptor 5-ht7, ou em ambos, em um indivíduo; método de fornecimento de atividade de antagonista funcional nos receptores adrenérgicos em um indivíduo |
| MX2019014272A (es) | 2017-06-01 | 2020-12-11 | Xoc Pharmaceuticals Inc | Compuestos policiclicos y usos de los mismos. |
| US11135379B2 (en) | 2019-02-15 | 2021-10-05 | Bn Intellectual Properties, Inc. | Method of delivering pharmaceutical products |
| US10758535B1 (en) * | 2019-04-26 | 2020-09-01 | Sumitomo Dainippon Pharma Co., Ltd. | Therapeutic drug for dyskinesia |
| US11559525B2 (en) | 2019-04-26 | 2023-01-24 | Sumitomo Pharma Co., Ltd. | Therapeutic drug for dyskinesia |
| US11364225B2 (en) * | 2019-08-21 | 2022-06-21 | Bn Intellectual Properties, Inc. | Pharmaceutical formulation for treating symptoms of migraine and cluster headaches, and method of using the same |
| JPWO2022045336A1 (cs) | 2020-08-31 | 2022-03-03 | ||
| IL307194A (en) * | 2021-03-25 | 2023-11-01 | Maplight Therapeutics Inc | Pharmaceutical compositions comprising zolmitriptan |
| WO2025164698A1 (ja) * | 2024-01-31 | 2025-08-07 | 株式会社ケイファーマ | ハンチントン病治療剤及び治療用組成物 |
| CN118308475B (zh) * | 2024-03-18 | 2024-11-26 | 安徽医科大学第一附属医院 | Htr1b作为胚胎发育停滞的诊断标志物和治疗靶点方面的应用 |
| EP4647069A1 (en) | 2024-05-07 | 2025-11-12 | Universita' Degli Studi Di Trieste | Drugs and compositions for use in the treatment of rett syndrome |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA200100089A1 (ru) * | 1998-07-30 | 2001-08-27 | Пфайзер Инк. | Предотвращение рецидива мигрени |
| WO2005034908A2 (en) * | 2003-10-10 | 2005-04-21 | Lifecycle Pharma A/S | A solid dosage form comprising a fibrate and a statin |
| RU2003138075A (ru) * | 2001-07-04 | 2005-06-10 | Сан Фармасьютикл Индастриз Лимитид (In) | Удерживаемая в желудке система регулируемой доставки лекарственного средства |
| WO2006027681A1 (en) * | 2004-09-07 | 2006-03-16 | Pfizer Limited | Combination of a 5-ht(1) receptor agonist and an alpha-2-delta ligand for the treatment of migraine |
| RU2322443C2 (ru) * | 2001-09-19 | 2008-04-20 | Мерк Патент Гмбх | Новое применение замещенных аминометилхроманов |
| WO2008047839A1 (en) * | 2006-10-19 | 2008-04-24 | Dainippon Sumitomo Pharma Co., Ltd. | 5-ht1a receptor agonist |
| EA200970022A1 (ru) * | 2006-06-16 | 2009-06-30 | Солвей Фармасьютикалс Б.В. | Комбинированные препараты, содержащие бифепрунокс и l-допу |
| WO2009118167A1 (de) * | 2008-03-25 | 2009-10-01 | Ratiopharm Gmbh | Pharmazeutische formulierung umfassend eine feste dispersion und verfahren zu deren herstellung |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE759371A (fr) | 1969-11-24 | 1971-05-24 | Bristol Myers Co | Azaspirodecanediones heterocycliques et procedes pour leur preparation |
| US3976776A (en) | 1972-12-06 | 1976-08-24 | Mead Johnson & Company | Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones |
| US4166452A (en) | 1976-05-03 | 1979-09-04 | Generales Constantine D J Jr | Apparatus for testing human responses to stimuli |
| US4182763A (en) | 1978-05-22 | 1980-01-08 | Mead Johnson & Company | Buspirone anti-anxiety method |
| US4356108A (en) | 1979-12-20 | 1982-10-26 | The Mead Corporation | Encapsulation process |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US4438119A (en) | 1982-12-23 | 1984-03-20 | Mead Johnson & Company | Method for alleviation of extrapyramidal motor disorders |
| US4640921A (en) | 1986-02-04 | 1987-02-03 | Bristol-Myers | Treatment of sexual dysfunction with buspirone |
| US4687772A (en) | 1986-10-07 | 1987-08-18 | Bristol-Myers Company | Method for improvement of short term memory |
| US4777173A (en) | 1987-03-25 | 1988-10-11 | Bristol-Myers Company | Method for treatment of alcohol abuse |
| US5185329A (en) | 1988-08-30 | 1993-02-09 | Bristol-Myers Squibb Company | Method for treatment of substance addiction |
| US6432956B1 (en) | 1990-02-12 | 2002-08-13 | William C. Dement | Method for treatment of sleep apneas |
| JP2738461B2 (ja) | 1990-06-07 | 1998-04-08 | ザ・ウエルカム・ファウンデーション・リミテッド | 治療用複素環化合物 |
| US5633009A (en) | 1990-11-28 | 1997-05-27 | Sano Corporation | Transdermal administration of azapirones |
| US5431922A (en) | 1991-03-05 | 1995-07-11 | Bristol-Myers Squibb Company | Method for administration of buspirone |
| DE4122217C2 (de) * | 1991-07-04 | 1997-02-13 | Merz & Co Gmbh & Co | Verfahren zur Herstellung mechanisch stabiler, gut zerfallender Komprimate aus kleinen wirkstoffhaltigen Formkörpern |
| GB9209882D0 (en) | 1992-05-07 | 1992-06-24 | Glaxo Lab Sa | Compositions |
| US5484788A (en) | 1993-03-26 | 1996-01-16 | Beth Israel Hospital Association | Buspirone as a systemic immunosuppressant |
| US5637314A (en) | 1995-06-07 | 1997-06-10 | Beth Israel Deaconess Medical Center, Inc. | Topical and systemic application of buspirone or derivatives thereof for treating atopic dermatitis |
| US6150365A (en) | 1999-08-05 | 2000-11-21 | Bristol-Myers Squibb Company | Anxiety method |
| GB9928578D0 (en) | 1999-12-03 | 2000-02-02 | Zeneca Ltd | Pharmaceutical formulations |
| ATE374192T1 (de) | 2000-11-29 | 2007-10-15 | Lilly Co Eli | 1-(2-m-methansulfonamidophenylethyl)-4-(m- trifluoromethylphenyl)piperazine und ihre akzeptablen pharmazeutischen salze und solvate und ihre verwendung zur behandlung von inkontinenz |
| AU2002241565A1 (en) | 2001-01-05 | 2002-07-16 | Eli Lilly And Company | Excitatory amino acid receptor antagonist and 5-ht1f agonist combination: a method for the treatment of neurological disorders |
| US8329734B2 (en) | 2009-07-27 | 2012-12-11 | Afgin Pharma Llc | Topical therapy for migraine |
| US7470435B2 (en) * | 2003-11-17 | 2008-12-30 | Andrx Pharmaceuticals, Llc | Extended release venlafaxine formulation |
| DE10353657A1 (de) | 2003-11-17 | 2005-06-23 | Merck Patent Gmbh | Indolderivate |
| EP1711493A2 (en) | 2004-02-06 | 2006-10-18 | CIBA SPECIALTY CHEMICALS HOLDING INC. Patent Departement | Crystalline forms of zolmitriptan |
| US8715727B2 (en) * | 2004-07-02 | 2014-05-06 | Shionogi Inc. | Tablet for pulsed delivery |
| KR20070087678A (ko) * | 2004-12-20 | 2007-08-28 | 컬리지움 파마슈티칼, 인코포레이티드 | 수면 장애용 약제 조성물 |
| AU2006206718B2 (en) * | 2005-01-18 | 2011-06-02 | Merck Sharp & Dohme Corp. | CGRP receptor antagonists |
| KR101406456B1 (ko) * | 2005-04-06 | 2014-06-20 | 아다마스 파마슈티칼스, 인코포레이티드 | Cns 장애의 치료를 위한 방법 및 조성물 |
| US20080166407A1 (en) * | 2005-07-29 | 2008-07-10 | Shalaby Shalaby W | Solid oral formulations for combination therapy |
| US9066903B2 (en) | 2006-02-28 | 2015-06-30 | The United States Of America As Represented By The Department Of Veterans Affairs | Pharmacological treatment of Parkinson's disease |
| WO2007129329A2 (en) * | 2006-05-08 | 2007-11-15 | Jubilant Organosys Limited | Extended release pharmaceutical formulation comprising venlafaxine hydrochloride |
| AU2007249435A1 (en) * | 2006-05-09 | 2007-11-22 | Braincells, Inc. | 5 HT receptor mediated neurogenesis |
| US20080069874A1 (en) * | 2006-09-15 | 2008-03-20 | Auriga Laboratories, Inc. | Kits for Prevention and Treatment of Rhinitis |
| EP2170282A4 (en) | 2007-06-27 | 2014-11-05 | Hanmi Pharm Ind Co Ltd | METHOD FOR PRODUCING A QUICKLY CRUSHING FORMULATION FOR ORAL ADMINISTRATION AND DEVICE FOR PREPARING AND PACKAGING THE FORMULATION |
| US20110183995A1 (en) | 2008-06-24 | 2011-07-28 | Neurosearch A/S | Eltoprazine for suppression of l-dopa induced dyskinesias |
| RU2011119494A (ru) | 2008-10-14 | 2012-11-27 | Макнейл Аб | Многокомпонентная интраоральная лекарственная форма препарата и ее применение |
| JP5723787B2 (ja) | 2009-01-23 | 2015-05-27 | アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニAziende Chimiche Riunite Angelini Francesco A.C.R.A.F.Societa Per Azioni | 制御放出の製剤処方または食品処方およびその製造方法 |
| WO2011079313A1 (en) | 2009-12-23 | 2011-06-30 | Map Pharmaceuticals, Inc. | Novel ergoline analogs |
| SI2627328T1 (sl) | 2010-10-15 | 2017-01-31 | Contera Pharma Aps | Kombinacije agonistov receptorjev serotonina za zdravljenje motenj premikanja |
| WO2012163365A1 (en) | 2011-06-01 | 2012-12-06 | Concit Pharma Aps | Combinations of serotonin receptor agonists for treatment of movement disorders |
-
2013
- 2013-04-18 NO NO13725557A patent/NO2838517T3/no unknown
- 2013-04-18 SG SG11201406690SA patent/SG11201406690SA/en unknown
- 2013-04-18 PT PT137255576T patent/PT2838517T/pt unknown
- 2013-04-18 EP EP13725557.6A patent/EP2838517B1/en active Active
- 2013-04-18 PL PL13725557T patent/PL2838517T3/pl unknown
- 2013-04-18 CN CN201380031301.4A patent/CN104411301B/zh active Active
- 2013-04-18 MY MYPI2014002948A patent/MY169068A/en unknown
- 2013-04-18 CA CA2870123A patent/CA2870123C/en active Active
- 2013-04-18 HU HUE13725557A patent/HUE037732T2/hu unknown
- 2013-04-18 MX MX2014012408A patent/MX361372B/es active IP Right Grant
- 2013-04-18 ES ES13725557.6T patent/ES2654787T3/es active Active
- 2013-04-18 RU RU2014145944A patent/RU2670272C2/ru active
- 2013-04-18 NZ NZ700474A patent/NZ700474A/en not_active IP Right Cessation
- 2013-04-18 BR BR112014025907-0A patent/BR112014025907B1/pt active IP Right Grant
- 2013-04-18 WO PCT/DK2013/050111 patent/WO2013156035A1/en not_active Ceased
- 2013-04-18 DK DK13725557.6T patent/DK2838517T3/en active
- 2013-04-18 IN IN9571DEN2014 patent/IN2014DN09571A/en unknown
- 2013-04-18 JP JP2015506098A patent/JP6216768B2/ja not_active Expired - Fee Related
- 2013-04-18 KR KR1020147032179A patent/KR102104635B1/ko active Active
- 2013-04-18 AU AU2013248685A patent/AU2013248685B2/en not_active Ceased
- 2013-04-18 US US14/395,134 patent/US10561618B2/en active Active
-
2014
- 2014-10-05 IL IL235000A patent/IL235000B/en active IP Right Grant
- 2014-10-17 PH PH12014502331A patent/PH12014502331B1/en unknown
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA200100089A1 (ru) * | 1998-07-30 | 2001-08-27 | Пфайзер Инк. | Предотвращение рецидива мигрени |
| RU2003138075A (ru) * | 2001-07-04 | 2005-06-10 | Сан Фармасьютикл Индастриз Лимитид (In) | Удерживаемая в желудке система регулируемой доставки лекарственного средства |
| RU2322443C2 (ru) * | 2001-09-19 | 2008-04-20 | Мерк Патент Гмбх | Новое применение замещенных аминометилхроманов |
| WO2005034908A2 (en) * | 2003-10-10 | 2005-04-21 | Lifecycle Pharma A/S | A solid dosage form comprising a fibrate and a statin |
| WO2006027681A1 (en) * | 2004-09-07 | 2006-03-16 | Pfizer Limited | Combination of a 5-ht(1) receptor agonist and an alpha-2-delta ligand for the treatment of migraine |
| EA200970022A1 (ru) * | 2006-06-16 | 2009-06-30 | Солвей Фармасьютикалс Б.В. | Комбинированные препараты, содержащие бифепрунокс и l-допу |
| WO2008047839A1 (en) * | 2006-10-19 | 2008-04-24 | Dainippon Sumitomo Pharma Co., Ltd. | 5-ht1a receptor agonist |
| WO2009118167A1 (de) * | 2008-03-25 | 2009-10-01 | Ratiopharm Gmbh | Pharmazeutische formulierung umfassend eine feste dispersion und verfahren zu deren herstellung |
Non-Patent Citations (3)
| Title |
|---|
| Munoz A. et al. Combined 5HT1A and 5HT1B receptor agonists for the treatment of L-DOPA-induced dskinesiam Brain 2008. - 131. - (Pt 12): 3380-94. * |
| Munoz A. et al. Combined 5HT1A and 5HT1B receptor agonists for the treatment of L-DOPA-induced dskinesiam Brain 2008. - 131. - (Pt 12): 3380-94. Raymond C Rowe, Paul J Sheskey, Marian E Quinn, Handbook of Pharmaceutical Excipients, No 6, 2009, P. 917, стр. 129-132, 326-327. * |
| Raymond C Rowe, Paul J Sheskey, Marian E Quinn, Handbook of Pharmaceutical Excipients, No 6, 2009, P. 917, стр. 129-132, 326-327. * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2813095C1 (ru) * | 2023-08-07 | 2024-02-06 | Непубличное акционерное общество "Северная звезда" | Фармацевтическая композиция, содержащая золмитриптан, и технология ее производства |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2670272C2 (ru) | Пероральная фармацевтическая композиция, подходящая для повышения эффективности лечения двигательных нарушений | |
| US20230078925A1 (en) | Pulsatile drug delivery system for treating morning akinesia | |
| JP2005506367A (ja) | 有効物質を徐放する3−(3−ジメチルアミノ−1−エチル−2−メチル−プロピル)フェノール含有医薬 | |
| JP2010530422A (ja) | うつ病のための組合せ治療 | |
| JP2013512252A5 (cs) | ||
| BRPI0708059A2 (pt) | formulação de niacina de baixo rubor | |
| EP3897641B1 (en) | Treatment of movement disorders | |
| JP2006514100A (ja) | 徐放性l−アルギニン製剤並びに製造方法および使用方法 | |
| JP2017519827A (ja) | ブスピロン代謝産物の使用 | |
| RU2642962C2 (ru) | Терапия болезни паркинсона с применением комбинации с фиксированными дозами | |
| US20140221385A1 (en) | Combinations of serotonin receptor agonists for treatment of movement disorders | |
| MXPA04009906A (es) | Composiciones farmaceuticas de liberacion controlada de carbipoda y levopoda. | |
| HK1207285B (en) | Orally available pharmaceutical formulation suitable for improved management of movement disorders | |
| RU2325905C2 (ru) | Содержащее 3-(3-диметиламино-1-этил-2-метилпропил)фенол лекарственное средство с замедленным высвобождением действующего вещества | |
| WO2005016319A2 (en) | Acute pharmacologic augmentation of psychotherapy with enhancers of learning or conditioning | |
| WO2007113371A1 (en) | Pharmaceutical composition and preparation method thereof | |
| HK1131888A (en) | Low flush niacin formulation | |
| HUE029193T2 (en) | Delayed release drug formulations of thiocolchicoside |